Synthesis of radiobrominated amino acid derivatives via silicon-bromine exchange reaction

渡辺 茂樹; 山田 圭一*; 渡邉 早貴*; 奥 浩之*; 森口 朋尚*; 篠塚 和夫*; 石岡 典子

no journal, , 

Br-76 (half-life: 16.1 h) is of interest for in vivo imaging using PET. Therefore, Br-76 labeled peptides which have high affinity to tumor cells are promising PET tracers for tumor imaging. Tin-halogen exchange reaction have been used for radiobromination. However, it is likely that synthesis of stannylated peptides is difficult because stannyl group is readily eliminated under acidic condition. Silicon-carbon bond is resistant to acid, leading us to employ silicon-bromine exchange reaction for the radiobromination. In this study, we are aiming to synthesize a radiobrominated phenylalanine derivative via the silicon-bromine exchange reaction as a feasible study.